EVIDENCE THAT 5‐METHOXY‐N, N‐DIMETHYL TRYPTAMINE IS A SPECIFIC SUBSTRATE FOR MAO‐A IN THE RAT: IMPLICATIONS FOR THE INDOLEAMINE DEPENDENT BEHAVIOURAL SYNDROME

@article{Squires1975EVIDENCET5,
  title={EVIDENCE THAT 5‐METHOXY‐N, N‐DIMETHYL TRYPTAMINE IS A SPECIFIC SUBSTRATE FOR MAO‐A IN THE RAT: IMPLICATIONS FOR THE INDOLEAMINE DEPENDENT BEHAVIOURAL SYNDROME},
  author={Richard Felt Squires},
  journal={Journal of Neurochemistry},
  year={1975},
  volume={24}
}
  • R. Squires
  • Published 1 January 1975
  • Biology, Chemistry
  • Journal of Neurochemistry
A simple method for the separation of 5‐hydroxyindoleacetic acid (5‐HIAA) and 5‐methoxyindoleacetic acid (5‐MeOIAA) on columns of non‐ionic polystyrene (Amberlite XAD‐2) is described. Administration of 5‐methoxy‐N, N‐dimethyl‐tryptamine (5‐MeODMT) 2 mg/kg i. p. to rats results in a sixfold increase in brain 5‐MeOIAA within 15 min. This increase is blocked by the selective inhibitor of MAO‐A, clorgyline, but not by the selective inhibitor of MAO‐B, deprenyl, indicating that 5‐MeODMT is… 
EFFECTS OF MONOAMINE OXIDASE INHIBITION BY CLORGYLINE, DEPRENIL OR TRANYLCYPROMINE ON 5‐HYDROXYTRYPTAMINE CONCENTRATIONS IN RAT BRAIN AND HYPERACTIVITY FOLLOWING SUBSEQUENT TRYPTOPHAN ADMINISTRATION
TLDR
It is concluded that while 5‐HT may normally be metabolized in the brain by ‘Type A’ MAO in vivo, when this form is inhibited,5‐HT can still be metabolitesized by ’Type B’ enzyme.
Behavioral effects of α,α,β,β-tetradeutero-5-MeO-DMT in rats: comparison with 5-MeO-DMT administered in combination with a monoamine oxidase inhibitor
TLDR
Deuterated tryptamines may be useful in behavioral and pharmacological studies to mimic the effects of tryptamine/MAOI combinations to indicate that the hyperactivity induced by 5- MeO-DMT after MAO inhibition is a consequence of reduced metabolism of 5-MeO- DMT, leading to prolonged occupation of central serotonin receptors.
Modification of the effects of 5-methoxy-N,N-dimethyltryptamine on exploratory behavior in rats by monoamine oxidase inhibitors
TLDR
The ability of harmaline to modify the behavioral effects of 5-MeO-DMT is mediated by the inhibition of MAOA, and 5-HT2A receptors are responsible for the late hyperactivity induced by 5- MeO- DMT in the presence ofMAOA inhibitors.
Behavioral and pharmacokinetic interactions between monoamine oxidase inhibitors and the hallucinogen 5-methoxy-N,N-dimethyltryptamine
  • A. Halberstadt
  • Biology, Psychology
    Pharmacology Biochemistry and Behavior
  • 2016
Nonlinear Pharmacokinetics of 5-Methoxy-N,N-dimethyltryptamine in Mice
TLDR
A nonlinear pharmacokinetic property for 5-MeO-DMT in mice is established, suggesting that the risk of 5-Methoxy-N,N,-dimethyltryptamine intoxication may be increased nonproportionally at higher doses.
SOME PARAMETERS AFFECTING THE ACTIVITY OF MONOAMINE OXIDASE IN PURIFIED BOVINE BRAIN MITOCHONDRIA 1
TLDR
The inhibition of kynuramine and serotonin deamination was non‐competitive but mixed competitive inhibition was found with tyramine and phenylethylamine, and pyrophosphate ion had little or no effect on MAO activity, regardless of substrate.
...
...

References

SHOWING 1-10 OF 10 REFERENCES
Inhibitory effect of chlorpromazine on the syndrome of hyperactivity produced by l‐tryptophan or 5‐methoxy‐N,N‐dimethyltryptamine in rats treated with a monoamine oxidase inhibitor
TLDR
The hyperactivity and hyperpyrexia produced by l‐tryptophan in rats treated with a monoamine oxidase inhibitor was inhibited by chlorpromazine, and Pretreatment of rats with p‐chlorophenylalanine did not inhibit hyperactivity produced by 5‐MeODMT.
A comparison of the pharmacological and biochemical properties of substrate‐selective monoamine oxidase inhibitors
TLDR
Antagonism of tetrabenazine sedation appears to be correlated with inhibition of the enzyme species that oxidize 5‐HT and NA but not with inhibition that oxidizes benzylamine, leading to the rise in brain 5‐ HT levels rather than NA levels.
STUDIES IN VIVO ON THE RELATIONSHIP BETWEEN BRAIN TRYPTOPHAN, BRAIN 5‐HT SYNTHESIS AND HYPERACTIVITY IN RATS TREATED WITH A MONOAMINE OXIDASE INHIBITOR AND L‐TRYPTOPHAN
TLDR
It is suggested that when monoamine oxidase is inhibited and the rate of 5‐HT synthesis is increased, granular uptake and storage of 5-HT and other rate‐limiting mechanisms for 5‐ht inactivation are unable to prevent 5‐ HT 'spilling over’ to produce hyperactivity.
Methyltetrahydrofolic Acid Mediates N- and O-Methylation of Biogenic Amines
TLDR
With methyltetrahydrofolic acid, serotonin is O-methylated to 5-methoxytryptamine, a novel indoleamine in mammalian brain.
Fluorimetric determination of 5-hydroxyindoleacetic acid in human urine and cerebrospinal fluid.
1971a) 1. Neurochem
  • 1971
1971b) Br
  • Pharmac
  • 1971